Macrocyclic peptides as drug candidates: recent progress and remaining challenges

AA Vinogradov, Y Yin, H Suga - Journal of the American Chemical …, 2019 - ACS Publications
Peptides as a therapeutic modality attract much attention due to their synthetic accessibility,
high degree of specific binding, and the ability to target protein surfaces traditionally …

Supramolecular luminescent sensors

TL Mako, JM Racicot, M Levine - Chemical reviews, 2018 - ACS Publications
There is great need for stand-alone luminescence-based chemosensors that exemplify
selectivity, sensitivity, and applicability and that overcome the challenges that arise from …

Orally absorbed cyclic peptides

DS Nielsen, NE Shepherd, W Xu, AJ Lucke… - Chemical …, 2017 - ACS Publications
Peptides and proteins are not orally bioavailable in mammals, although a few peptides are
intestinally absorbed in small amounts. Polypeptides are generally too large and polar to …

[HTML][HTML] Systemic delivery of peptides by the oral route: Formulation and medicinal chemistry approaches

DJ Brayden, TA Hill, DP Fairlie, S Maher… - Advanced drug delivery …, 2020 - Elsevier
In its 33 years, ADDR has published regularly on the po5tential of oral delivery of biologics
especially peptides and proteins. In the intervening period, analysis of the preclinical and …

Cyclic peptides as drugs for intracellular targets: the next frontier in peptide therapeutic development

LK Buckton, MN Rahimi… - Chemistry–A European …, 2021 - Wiley Online Library
Developing macrocyclic peptides that can reach intracellular targets is a significant
challenge. This review discusses the most recent strategies used to develop cell permeable …

Strategies for fine-tuning the conformations of cyclic peptides

R Jwad, D Weissberger, L Hunter - Chemical Reviews, 2020 - ACS Publications
Cyclic peptides are promising scaffolds for drug development, attributable in part to their
increased conformational order compared to linear peptides. However, when optimizing the …

Lipophilic permeability efficiency reconciles the opposing roles of lipophilicity in membrane permeability and aqueous solubility

MR Naylor, AM Ly, MJ Handford… - Journal of medicinal …, 2018 - ACS Publications
As drug discovery moves increasingly toward previously “undruggable” targets such as
protein–protein interactions, lead compounds are becoming larger and more lipophilic …

Improving drug design: an update on recent applications of efficiency metrics, strategies for replacing problematic elements, and compounds in nontraditional drug …

NA Meanwell - Chemical Research in Toxicology, 2016 - ACS Publications
Drug discovery and development is a complex and lengthy enterprise that suffers from high
rates of candidate attrition at all stages of the process. The physical, biological, and …

Cyclic and macrocyclic peptides as chemical tools to recognise protein surfaces and probe protein–protein interactions

TAF Cardote, A Ciulli - ChemMedChem, 2016 - Wiley Online Library
Targeting protein surfaces and protein–protein interactions (PPIs) with small molecules is a
frontier goal of chemical biology and provides attractive therapeutic opportunities in drug …

Conformational Control of Macrocycles by Remote Structural Modification: Focus Review

SD Appavoo, S Huh, DB Diaz, AK Yudin - Chemical reviews, 2019 - ACS Publications
The conformational analysis of macrocycles is a complex and challenging problem. There
are many factors that contribute to this complexity. These include a large number of degrees …